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2c6e

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Revision as of 23:17, 30 March 2008 by OCA (Talk | contribs)
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Image:2c6e.gif


PDB ID 2c6e

Drag the structure with the mouse to rotate
, resolution 2.1Å
Sites:
Ligands:
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



AURORA A KINASE ACTIVATED MUTANT (T287D) IN COMPLEX WITH A 5-AMINOPYRIMIDINYL QUINAZOLINE INHIBITOR


Overview

A novel series of 5-aminopyrimidinyl quinazolines has been developed from anilino-quinazoline 1, which was identified in a high throughput screen for Aurora A. Introduction of the pyrimidine ring and optimisation of the substituents both on this ring and at the C7 position of the quinazoline led to the discovery of compounds that are highly specific Aurora kinase inhibitors. Co-crystallisation of one of these inhibitors with a fragment of Aurora A shows the importance of the benzamido group in achieving selectivity.

About this Structure

2C6E is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors., Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S, Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. Epub 2005 Dec 5. PMID:16337122

Page seeded by OCA on Mon Mar 31 02:16:59 2008

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